Pickering Emulsions Stabilized by Calcium Carbonate Particles: A New Topical Formulation

© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).Pickering emulsions are systems composed of two immiscible fluids stabilized by solid organic or inorganic particles. Pickering emulsions are particularly useful in cosmetics, where the surfactants are unwanted, as well as in the pharmaceutical field, where transdermal and/or dermal drug delivery is difficult to achieve and controlled drug release is desired. Here, we studied calcium carbonate particles as stabilizers of Pickering emulsions for topical use. An optimized formulation was obtained using a Quality by Design approach. First, a screening experiment was performed to identify the formulation and process critical variables that affect the quality properties of the Pickering emulsion. The optimization of the production was then studied by establishing the design space. The final formulation was hereinafter investigated regarding the pH, rheological properties, and in vitro cytotoxicity assays. The results showed the formulation had a pH compatible with human skin and a shear thinning behavior. Moreover, this formulation showed a strong network structure, with a suitable spreadability on the skin, allowing an easy application. The in vitro assays were performed to assess the potential cytotoxicity of the calcium carbonate-stabilized emulsion and the particles themselves, and the results revealed that the formulation did not significantly affect the cell viability. In conclusion, the use of calcium carbonate particles as a stabilizer ingredient contributed to achieve an eco-friendly Pickering emulsion.This research was funded by Fundação para a Ciência e a Tecnologia, Portugal (UID/DTP/04138/2019, PTDC/MEC-DER/30198/2017, and CEECINST/00145/2018) and by Carbomin.info:eu-repo/semantics/publishedVersio

Evaluating the presence of lycopene-enriched extracts from tomato on topical emulsions: Physico-chemical characterization and sensory analysis

UIDB/QUI/50006/2020 UIDB/04138/2020 UIDP/04138/2020 PTDC/SAU-SER/30197/2017LISBOA-01-0145-FEDER-030197 IF/01146/2015One of the new trends of personal care industry is the use of organic ingredients derived from nature, in particular, from food-processing residues with proven efficacy. Lycopene is a carotenoid responsible for the red color of several fruits, namely tomato, whose antioxidant and photoprotective effects have been studied. Methods: Lycopene-enriched extracts (LEE) were obtained from tomato waste using supercritical CO2 extraction, incorporated in microemulsions and macroemulsions for topical use, and characterized through GC-MS for the identification of volatile compounds. The aim of this work was to evaluate the impact of the presence of lycopene-enriched extracts developed emulsions through the identification of volatile compounds and by a sensory analysis to assess the odor and color perception and the acceptability of such semi-solid systems as cosmetic products. Results: Volatile compounds were identified in the extract and in the formulations containing the extract. Preliminary data show that the odor of both LEE-loaded microemulsions and LEE-loaded macroemulsions was classified as undefined. The information about the composition did not modify the odor perception but increased the acceptability of some cosmetic products. LEE conferred a yellowish color to formulations, and the information about the formulation composition increased the likelihood of different cosmetic products with this color being bought. Conclusions: The commercialization of personal care products does not only dependent on the associated organoleptic properties, but is influenced by the information about the composition, namely by the presence of an antioxidant compound.publishersversionpublishe

Investigations of olive oil industry by-products extracts with potential skin benefits in topical formulations

Funding Information: This work was supported by Sovena Portugal Consumer Goods through the project 569 Oil4Health: From Olive to Health LISBOA-01-0247-FEDER-038554, funded by the 570 Portugal 2020 program?Programa Operacional Regional de Lisboa. This research was also funded by FCT (Funda??o para a Ci?ncia e a Tecnologia) through iMed.ULisboa UID/DTP/04138/2019 and UIDB/04138/2020), principal investigator grants CEECIND/03143/2017 (L. M. Gon?alves). Joana Marto is financed through FCT, I.P., under the Scientific Employment Stimulus?Institutional Call (CEECINST/00145/2018). Marta Martins is financed through FCT, I.P., under the Scientific Employment Stimulus?Institutional Call (CEECINST/00102/2018). The work was supported by the Marine and Environmental Sciences Centre?MARE (UIDB04292/2020; UIDP/04292/2020). Funding Information: Funding: This work was supported by Sovena Portugal Consumer Goods through the project 569 Oil4Health: From Olive to Health LISBOA-01-0247-FEDER-038554, funded by the 570 Portugal 2020 program—Programa Operacional Regional de Lisboa. This research was also funded by FCT (Fundação para a Ciência e a Tecnologia) through iMed.ULisboa UID/DTP/04138/2019 and UIDB/04138/2020), principal investigator grants CEECIND/03143/2017 (L. M. Gonçalves). Joana Marto is financed through FCT, I.P., under the Scientific Employment Stimulus—Institutional Call (CEECINST/00145/2018). Marta Martins is financed through FCT, I.P., under the Scientific Employment Stimulus—Institutional Call (CEECINST/00102/2018). The work was supported by the Marine and Environmental Sciences Centre—MARE (UIDB04292/2020; UIDP/04292/2020). Publisher Copyright: © 2021 by the authors. Licensee MDPI, Basel, Switzerland.The by-products of olive oil industry are a major ecological issue due to their phenolic content, highly toxic organic load, and low pH. However, they can be recovered and reused, since their components have antioxidant, anti-inflammatory, and photoprotector properties. In this work, oil-in-water creams containing three different olive oil industry by-products extracts were produced without the use of organic solvents. First, the extracts were thoroughly characterized in vitro for cytotoxicity, inhibition of skin enzymes, and antioxidant and photoprotection capacities. Safety studies were then performed, including ocular and skin irritation tests, ecotoxicity evaluation, and in vivo Human Repeat Insult Patch Test. The results obtained in this initial characterization supported the incorporation of the extracts in the cream formulations. After preparation, the creams were characterized for their organoleptic, physicochemical, droplet size and rheological properties, and microbial contamination. The results showed that all formulations were semi-solid creams, with stable pH, compatible with the skin, without microbial contamination, and with the expected droplet size range. The rheological analysis showed shear-thinning behavior with yield stress, with the viscosity decreasing with increasing shear rate. The oscillatory results suggest that the creams have a strong network structure, being easily rubbed into the skin. Finally, compatibility, acceptability and antioxidant efficacy were evaluated in vivo, in human volunteers. No adverse reactions were observed after application of the formulations on skin and the cream with the highest concentrations of phenolic compounds showed the highest antioxidant efficiency. In conclusion, the results suggest that olive oil industry by-products extracts have valuable properties that favor their re-use in the cosmetic industry. The example presented here showed their successful incorporation into creams and their impact in these formulations’ appearance, pH, and rheological performance, as well as their in vivo compatibility with skin and antioxidant efficiency.publishersversionpublishe

Development and characterization of novel vehicles for topical drug delivery

Tese de doutoramento, Farmácia (Tecnologia Farmacêutica), Universidade de Lisboa, Faculdade de Farmácia, 2016Topical drug delivery is challenging since the skin acts as a natural and protective barrier. The skin has been an important route for drug delivery when topical, local or systemic effects are desired. The outcome of topical dermatological drug treatment is significantly influenced by the choice of vehicle. In recent years there has been an increased interest in developing improved delivery systems and, exploring new ways of using approved excipients, such as, starch. Due to its unique properties, starch has been extensively used in various topical pharmaceutical application, i.e. as a sensorial enhancer, a stabilizer and drug delivery polymer, providing protection and control release of the drug molecule. The base-concept of this study was to develop and characterize novel starch-based vehicles for dermatological application, easily scaled-up to industry and produced by methods that can allow the decrease of production costs, and further investigate the resulting systems behavior in in vitro and in vivo conditions. Starch-based vehicles were prepared successfully using QbD approach with the understanding of the high risk process and formulation parameters involved and optimized design space with a multifactorial combination of critical parameters to obtain predetermined specifications. Three different model drugs were incorporated into the optimized starch-based vehicles. Minocycline hydrochloride (MH) was incorporated in Pickering emulsions, a human neutrophil elastase inhibitor (ER143), a new molecule developed by the MedChem Group at iMed.ULisboa, was encapsulated into starch nanocapsules and melatonin was added on Pickering emulsions sunscreen, in order to fully characterize these new formulations, and further study its topical delivery and in vitro and in vivo efficacy. The in vitro antibacterial activity studies for Pickering emulsions containing MH revealed that the released drug exceeded the minimum inhibitory concentration of MH against S.aureus. In vitro release studies showed a prolonged release of the MH, with an initial burst effect. Regarding in vitro permeation studies, MH does not pass through the entire skin layer, suggesting a minimal potential for the systemic absorption of the MH upon topical administration. In vivo results showed that topical administration of MH was effective in S. aureus superficial infections treatment. Starch nanocapsules presented a mean particle size ranging from 200 to 250 nm and a positive zeta potential. In vitro permeation studies showed that the starch nanocapsules were suitable for the delivery of ER143, allowing a high control of the drug release, contributing to a high skin retention and/or permeation profiles of ER143. In vivo results showed that erythema and edema were attenuated in 98%, following the local application of ER143-loaded starch nanocapsules. Regarding Pickering emulsions sunscreen, formulation studies demonstrated that starch particles presented no intrinsic photoprotection properties, they proved to be a sun protection factor promoter by a synergistic effect. Besides the excellent sunscreen activity confirmed by in vitro and in vivo results, the final formulations proved to be also suitable for topical use according to the rheological assessment and stability throughout the study period (3 months). Additionally, the safety and biological effects of the placebos (vehicles without drug) was assessed by using both in vitro and in vivo studies, as an adequate equilibrium between the safety and efficacy effects. Overall, these findings highlight the starch-based vehicles as promising for the development of topical delivery systems, covering innovative therapeutic approaches

Sugar Surfactant-Based Shampoos

© 2020 AOCSNaturally derived surfactants in hair care products are a trend in cosmetic technology. This study aimed to formulate and fully characterize the performance of shampoos with sugar-derived surfactants, namely, the alkyl polyglucosides decyl glucoside and coco-glucoside. In addition, different thickeners and conditioning ingredients were added to improve the formulation properties. A sodium laureth sulfate (SLES) formulation was used as control. Rheology, pH, foaming, contact angles on a keratin surface, and surface tensions were determined. The safety of the formulations was evaluated by in vitro cytotoxicity studies using the human keratinocyte HaCaT cell line and human retinal pigment epithelial cells ARPE-19. The efficacies were studied by in vitro hair combing force assays and in vivo sensorial analysis. The formulated sugar surfactant-based shampoos showed the following properties: (i) pH values higher than those of SLES (which were posteriorly lowered with lactic acid); (ii) higher foamability than SLES, and high wettability; (iii) Newtonian behavior and predominance of liquid state with a suitable viscosity; (iv) low cytotoxicity in both human keratinocytes and retinal cell lines (in contrast to SLES); (v) easier hair combing than SLES, when Polyquaternium-7 was used as conditioner; (vi) efficient and gentle hair washing; and (vii) favorable sensorial analysis confirming the previous washing properties. In conclusion, the sugar surfactants had a considerable impact in the properties of the shampoo formulations, in terms of both hair cleansing properties and efficacy, as demonstrated here. These favorable outcomes clearly support the use of these ingredients in shampoo formulation design.This research was funded by Fundação para a Ciência e a Tecnologia, Portugal (UID/DTP/04138/2019 to iMed.Ulisboa and SFRH/BSAB/150315/2019 to Andreia Ascenso).info:eu-repo/semantics/publishedVersio

Pickering Emulsions Stabilized by Calcium Carbonate Particles: A New Topical Formulation

Pickering emulsions are systems composed of two immiscible fluids stabilized by solid organic or inorganic particles. Pickering emulsions are particularly useful in cosmetics, where the surfactants are unwanted, as well as in the pharmaceutical field, where transdermal and/or dermal drug delivery is difficult to achieve and controlled drug release is desired. Here, we studied calcium carbonate particles as stabilizers of Pickering emulsions for topical use. An optimized formulation was obtained using a Quality by Design approach. First, a screening experiment was performed to identify the formulation and process critical variables that affect the quality properties of the Pickering emulsion. The optimization of the production was then studied by establishing the design space. The final formulation was hereinafter investigated regarding the pH, rheological properties, and in vitro cytotoxicity assays. The results showed the formulation had a pH compatible with human skin and a shear thinning behavior. Moreover, this formulation showed a strong network structure, with a suitable spreadability on the skin, allowing an easy application. The in vitro assays were performed to assess the potential cytotoxicity of the calcium carbonate-stabilized emulsion and the particles themselves, and the results revealed that the formulation did not significantly affect the cell viability. In conclusion, the use of calcium carbonate particles as a stabilizer ingredient contributed to achieve an eco-friendly Pickering emulsion

Rheology as a Tool to Predict the Release of Alpha-Lipoic Acid from Emulsions Used for the Prevention of Skin Aging

The availability of an active substance through the skin depends basically on two consecutive steps: the release of this substance from the vehicle and its subsequent permeation through the skin. Hence, studies on the specific properties of vehicles, such as their rheological behavior, are of great interest in the field of dermatological products. Recent studies have shown the influence of the rheological features of a vehicle on the release of drugs and active compounds from the formulation. In this context, the aim of this study was to evaluate the influence of the rheological features of two different emulsion formulations on the release of alpha-lipoic acid. Alpha-lipoic acid (ALA) was chosen for this study because of its antioxidant characteristics, which could be useful for the prevention of skin diseases and aging. The rheological and mechanical behavior and the in vitro release profile were assayed. The results showed that rheological features, such as viscosity, thixotropy, and compliance, strongly influenced the release of ALA from the emulsion and that the presence of a hydrophilic polymer in one of the emulsions was an important factor affecting the rheology and, therefore, the release of ALA

Sustainable valorization of food-processing industry by-products: challenges and opportunities to obtain bioactive compounds

Copyright © 2021 Elsevier Inc. All rights reserved.The food-processing industry generates large quantities of residues, which may represent sustainable and rich sources of bioactive compounds. The extraction of bioactives from industrial residues could be a good alternative for the valorization of this by-product with recognized biological actions. Conventional extraction methods consume large volumes of organic solvents, which are expensive, toxic, and hazardous. Traces of the extractants in the final product make it unsuitable for pharmaceutical or cosmetic uses. Several methods, considered “green” or “eco-friendly,” have been proposed because of the low contamination, nontoxic, and nonflammable characteristics of the techniques. This chapter reviews the use of bioactive-enriched extracts obtained by environmentally friendly processes with sufficient quality to be incorporated into nutraceutical, pharmaceutical, and cosmetic formulations, highlights the challenges regarding bioactive compounds’ chemical stability, and presents the more recent strategies to overcome the technological issues of extracted bioactive molecules. The new concepts for recovered bioactives application are discussed.info:eu-repo/semantics/publishedVersio

In Vitro Characterization of Reversine-Treated Gingival Fibroblasts and Their Safety Evaluation after In Vivo Transplantation

Reversine is a purine derivative that has been investigated with regard to its biological effects, such as its anticancer properties and, mostly, its ability to induce the dedifferentiation of adult cells, increasing their plasticity. The obtained dedifferentiated cells have a high potential for use in regenerative procedures, such as regenerative dentistry (RD). Instead of replacing the lost or damaged oral tissues with synthetic materials, RD uses stem cells combined with matrices and an appropriate microenvironment to achieve tissue regeneration. However, the currently available stem cell sources present limitations, thus restricting the potential of RD. Based on this problem, new sources of stem cells are fundamental. This work aims to characterize mouse gingival fibroblasts (GFs) after dedifferentiation with reversine. Different administration protocols were tested, and the cells obtained were evaluated regarding their cell metabolism, protein and DNA contents, cell cycle changes, morphology, cell death, genotoxicity, and acquisition of stem cell characteristics. Additionally, their teratoma potential was evaluated after in vivo transplantation. Reversine caused toxicity at higher concentrations, with decreased cell metabolic activity and protein content. The cells obtained displayed polyploidy, a cycle arrest in the G2/M phase, and showed an enlarged size. Additionally, apoptosis and genotoxicity were found at higher reversine concentrations. A subpopulation of the GFs possessed stem properties, as supported by the increased expression of CD90, CD105, and TERT, the existence of a CD106+ population, and their trilineage differentiation capacity. The dedifferentiated cells did not induce teratoma formation. The extensive characterization performed shows that significant functional, morphological, and genetic changes occur during the dedifferentiation process. The dedifferentiated cells have some stem-like characteristics, which are of interest for RD